Synthesis and Evaluation of Novel N-Substituted-6-methoxynaphthalene-2-Carboxamides as Potential Chemosensitizing Agents for Cancer

Abstract

A novel class of molecules with structure N-[3-(heteroaryl)propyl]-6-methoxynaphthalene-2-carboxamides 8—13 were synthesized by condensing 6-methoxy-2-naphthoyl chloride 1 with 3-(heteroaryl)propyl amines 2—7. Compounds 8—12 were evaluated in vitro, in P388 murine lymphocytic leukemia cell line (P388) using SRB assay for cytotoxicity and in adriamycin resistant P388 murine lymphocytic leukemia cell line (P388/ADR) using MTT assay for resistant reversal activity. Compounds 8—12 were non-toxic at lower dose of 20 μg/ml, and effectively reversed adriamycin resistance. However, at higher doses (40, 80 μg/ml) they showed significant cytotxicity and hence reversal potency was not determined at these concentrations.